In rat basophilic leukemia cells (2H3), a tumor analog of mast cells, the aggregation of IgE receptors results in histamine secretion and the increase in histidine decarboxylase activity which synthesizes histamine. Using inhibitors of protein kinases C, we studied the relationships between these events and protein kinase C which is activated by antigens. Histamine release is suppressed by inhi...

Mitosis entails mechanistic changes required for maintaining the genomic integrity in all dividing cells. The process is intricate and temporally spatially regulated by ordered series of activation de-activation protein kinases. mitotic kinases ensure stepwise progression entry into mitosis after G2 phase cell cycle, followed prophase, pro-metaphase, metaphase, anaphase, telophase, subsequently...

Protein kinases exist in equilibrium of active and inactive states, in which the aspartate-phenylalanine-glycine motif in the catalytic domain undergoes conformational changes that are required for function. Drugs targeting protein kinases typically bind the primary ATP-binding site of an active state (type-I inhibitors) or utilize an allosteric pocket adjacent to the ATP-binding site in the in...

The specific phosphoinositide 3-kinase (PI3K) inhibitors wortmannin and LY294002 have been invaluable tools for elucidating the roles of these enzymes in signal transduction pathways. The X-ray crystallographic structures of PI3Kgamma bound to these lipid kinase inhibitors and to the broad-spectrum protein kinase inhibitors quercetin, myricetin, and staurosporine reveal how these compounds fit ...

Neurite outgrowth is important in neuronal circuit formation and functions, for regeneration of networks following trauma disease the brain. Thus, identification characterization molecules that regulate neurite are essential understanding how brain circuits form function development treatment neurological disorders. In this study, we found structurally different lysophosphatidylethanolamine (LP...

EGFR is a key player in the signalling cascades of various kinds cancers and tyrosine kinase inhibitors block signalling. Natural products have long been used as candidates for therapy management cancer. Violacein, bacterial pigment, has known its numerous biological applications such antimicrobial, antileishmanial, antiviral, well antitumoral. Computational studies concluded that it may activi...

A human monocytic cell line, THP-1, stimulated with 40 nM phorbol myristate acetate (PMA), differentiated to macrophage-like cells, and exhibited increased expression and release of interleukin-10 and expression of acetylated low density lipoprotein (ac-LDL) receptors. A selective inhibitor, MDL 29,152 (4-propyl-5-(4-quinolinyl)-2(3H)-oxazolone) was used to show that this induction required act...

The potent natural toxins microcystin, nodularin, and okadaic acid act rapidly to induce apoptotic cell death. Here we show that the apoptosis correlates with protein phosphorylation events and can be blocked by protein kinase inhibitors directed against the multifunctional Ca(2+)/calmodulin-dependent protein kinase II (CaMKII). The inhibitors used comprised a battery of cell-permeable protein ...